2018
DOI: 10.1002/ardp.201700304
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Synthesis, p38α MAP kinase inhibition, anti‐inflammatory activity, and molecular docking studies of 1,2,4‐triazole‐based benzothiazole‐2‐amines

Abstract: Recent studies have demonstrated that inhibition of p38α MAP kinase could effectively inhibit pro-inflammatory cytokines including TNF-α and interleukins. Thus, inhibition of this enzyme can prove greatly beneficial in the therapy of chronic inflammatory diseases. A new series of N-[3-(substituted-4H-1,2,4-triazol-4-yl)]-benzo[d]thiazol-2-amines (4a-n) were synthesized and subjected to in vitro evaluation for anti-inflammatory activity (BSA anti-denaturation assay) and p38α MAPK inhibition. Among the compounds… Show more

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Cited by 32 publications
(26 citation statements)
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“…N ‐[3‐(Substituted‐4 H ‐1,2,4‐triazol‐4‐yl)]benzo[ d ]thiazol‐2‐amines were synthesized by Tariq et al The synthesized compounds were screened for anti‐inflammatory activity and p38α MAPK inhibition. Compound 14 was found to be the most active with an in vivo anti‐inflammatory efficacy of 85.31% when compared to diclofenac sodium (83.68%).…”
Section: Biological Applications Of Benzothiazole Derivativesmentioning
confidence: 99%
See 1 more Smart Citation
“…N ‐[3‐(Substituted‐4 H ‐1,2,4‐triazol‐4‐yl)]benzo[ d ]thiazol‐2‐amines were synthesized by Tariq et al The synthesized compounds were screened for anti‐inflammatory activity and p38α MAPK inhibition. Compound 14 was found to be the most active with an in vivo anti‐inflammatory efficacy of 85.31% when compared to diclofenac sodium (83.68%).…”
Section: Biological Applications Of Benzothiazole Derivativesmentioning
confidence: 99%
“…Docked pose of compound 14 , represented as dark turquoise color tube in the binding site of p38α MAP kinase showing hydrogen bond interactions (red dash lines)…”
Section: Biological Applications Of Benzothiazole Derivativesmentioning
confidence: 99%
“…PAK4 Sep474 binding was observed with piperidinecarbonitrile, acetamide and urea derivatives at ATP-binding groove. In contrast, inactive PAK4 binding was prominent with pyrimidinone, pyrazinecarboxamide and acrylamide derivatives [56]. Thus ATP-competitive inhibitors may prove ideal therapeutic choice for PAK family members.…”
Section: Discussionmentioning
confidence: 99%
“…46 ) were synthesized and evaluated for their in vitro anti-inflammatory activity and p38α MAP kinase inhibition by Tariq et al. [ 221 , 222 ]. Among the selected compounds for in vivo evaluation, compounds 249a and 250a emerged as the most potent compound with edema inhibition of 84.43% and 85.31%, respectively.…”
Section: Biological Activities Of 124-triazole Derivativesmentioning
confidence: 99%